- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實驗
- Cell Counting Kit-8 (CCK-8)
- 新產(chǎn)品
- 聯(lián)系我們
IPA-3
IPA-3是一種選擇性的，非ATP競爭性Pak1抑制劑，無細(xì)胞試驗中IC50為2.5 μM，對第II組PAKs(PAKs 4-6)沒有抑制作用。
IPA-3 Chemical Structure
CAS: 42521-82-4
產(chǎn)品質(zhì)控
批次：
S709301
DMSO]70 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false
純度：
99.66%
99.66
IPA-3相關(guān)產(chǎn)品
| 相關(guān)靶點 | PAK1 PAK3 PAK2 PAK4 PAK5 PAK6 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | FRAX597 PF-3758309 FRAX486 FRAX1036 LCH-7749944 NVS-PAK1-1 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫 細(xì)胞骨架信號通路化合物庫 抗心血管疾病化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| human NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.97694 μM | |||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.17833 μM | |||
| human YT cell | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=1.39036 μM | |||
| human BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.03796 μM | |||
| human SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=2.10219 μM | |||
| human MCF7 cell | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=2.1807 μM | |||
| human GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=2.63494 μM | |||
| human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.7595 μM | |||
| human QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=2.90891 μM | |||
| human BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=3.09844 μM | |||
| human CMK cell | Growth inhibition assay | Inhibition of human CMK cell growth in a cell viability assay, IC50=3.14599 μM | |||
| human U-698-M cell | Growth inhibition assay | Inhibition of human U-698-M cell growth in a cell viability assay, IC50=3.23856 μM | |||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=3.24662 μM | |||
| human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=3.31805 μM | |||
| human REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay, IC50=3.36655 μM | |||
| human MHH-PREB-1 cell | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=3.46687 μM | |||
| human KE-37 cell growth | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=3.50231 μM | |||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=3.54519 μM | |||
| human CA46 cell | Growth inhibition assay | Inhibition of human CA46 cell growth in a cell viability assay, IC50=3.6618 μM | |||
| human HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50=3.72768 μM | |||
| human NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50=3.83751 μM | |||
| human 8305C cell | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=4.16758 μM | |||
| human EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=4.20148 μM | |||
| human NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=4.2256 μM | |||
| human EB2 cell | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=4.49142 μM | |||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay | |||
| human HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=4.52149 μM | |||
| human ST486 cell | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=4.8654 μM | |||
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=5.04354 μM | |||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=5.1176 μM | |||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.14768 μM | |||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=5.28471 μM | |||
| human PF-382 | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=5.35226 μM | |||
| human SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=5.37256 μM | |||
| human WSU-NHL cell | Growth inhibition assay | Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=5.52067 μM | |||
| human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=5.6414 μM | |||
| human Daudi cell | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=5.68477 μM | |||
| human MC-CAR cell | Growth inhibition assay | Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=5.70644 μM | |||
| human RPMI-8402 cell | Growth inhibition assay | Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=5.76876 μM | |||
| human CCRF-CEM cell | Growth inhibition assay | Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=5.97667 μM | |||
| human CHP-126 cell | Growth inhibition assay | Inhibition of human CHP-126 cell growth in a cell viability assay, IC50=6.74268 μM | |||
| human NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=6.76352 μM | |||
| human KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=6.88549 μM | |||
| human J82 cell | Growth inhibition assay | Inhibition of human J82 cell growth in a cell viability assay, IC50=7.04965 μM | |||
| human SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=7.83558 μM | |||
| human HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50=8.06805 μM | |||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=8.21464 μM | |||
| human HL-60 cell | Growth inhibition assay | Inhibition of human HL-60 cell growth in a cell viability assay, IC50=8.84605 μM | |||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=9.1649 μM | |||
| human SK-N-DZ cell | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.20423 μM | |||
| human HT-1197 cell | Growth inhibition assay | Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=10.3073 μM | |||
| human NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.7152 μM | |||
| human HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=18.6283 μM | |||
| human SK-LU-1 cell | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=18.8731 μM | |||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=21.8897 μM | |||
| human A2780 cell | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM | |||
| 點擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | IPA-3是一種選擇性的，非ATP競爭性Pak1抑制劑，無細(xì)胞試驗中IC50為2.5 μM，對第II組PAKs(PAKs 4-6)沒有抑制作用。 | ||
|---|---|---|---|
| 特性 | IPA-3共價結(jié)合到Pak1的調(diào)節(jié)域，并抑制結(jié)合到Cdc42的上游活化劑。 | ||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | IPA-3是非ATP競爭性的p21-激活激酶1(Pak1)的變構(gòu)抑制劑。IPA-3抑制Cdc42刺激的Pak1在Thr423位點自磷酸化。IPA-3也抑制鞘氨醇依賴性的Pak1自磷酸化。IPA-3不靶向作用于暴露的Pak1的半胱氨酸殘基。IPA-3的二硫鍵對抑制Pak1是至關(guān)重要的，且通過還原劑二硫蘇糖醇（DTT）廢除IPA-3對Pak1的抑制。IPA-3通過不同的活化劑抑制Pak1激活, 但不抑制預(yù)活化的Pak1。IPA-3作用于小鼠胚胎成纖維細(xì)胞，抑制PDGF刺激的Pak激活。[1]IPA-3通過共價結(jié)合到Pak1的調(diào)節(jié)域抑制Pak1活化。IPA-3與Pak1共價結(jié)合，這種作用存在時間和溫度依賴性。IPA-3抑制Pak1活化劑Cdc42的結(jié)合。IPA-3直接結(jié)合到Pak1的自動調(diào)節(jié)域。IPA-3 作用于細(xì)胞，可逆抑制PMA誘導(dǎo)的膜皺裂。[2] | |||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | p-PAK1 / PAK1 / p-PAK2 / PAK2 / p-Raf1 / Raf1 / p-MEK1 / MEK1 / p-ERK / ERK |
|
30971268 | |
| Growth inhibition assay | Cell viability |
|
30971268 | |
| Immunofluorescence | Paxillin NF-κB BiP |
|
23894351 | |
|
化學(xué)信息&溶解度
| 分子量 | 350.45 | 分子式 | C20H14O2S2 |
| CAS號 | 42521-82-4 | SDF | Download IPA-3 SDF |
| Smiles | C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 70 mg/mL ( (199.74 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 7 mg/mL (19.97 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術(shù)支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
常見問題及建議解決方法
問題 1:
If this product is cell membrane permeable and would it be suitable for PAK1 inhibition on a pancreatic beta cell line?
回答：
Based on the reference, I think IPA-3 is able to penetrate the cell membrane, it's likely to inhibit PAK1 on a pancreatic beta cell line although there is no reference confirming it: Figure 3: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963893/; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4353635/
